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5-HT1D receptor

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Target not currently curated in GtoImmuPdb

Target id: 3

Nomenclature: 5-HT1D receptor

Family: 5-Hydroxytryptamine receptors

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 377 1p36.12 HTR1D 5-hydroxytryptamine receptor 1D 49
Mouse 7 374 4 68.74 cM Htr1d 5-hydroxytryptamine (serotonin) receptor 1D 50
Rat 7 374 5q36 Htr1d 5-hydroxytryptamine receptor 1D 11
Previous and Unofficial Names Click here for help
5-HT1Dα [49] | HTRL | 5-HT1D | HT1DA | serotonin receptor 1D | Gpcr14 | Htr1db | 5-hydroxytryptamine (serotonin) receptor 1D, G protein-coupled
Database Links Click here for help
Specialist databases
GPCRDB 5ht1d_human (Hs), 5ht1d_mouse (Mm), 5ht1d_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands Click here for help
5-HT-moduline
5-hydroxytryptamine

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]eletriptan Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 9.1 pKd 29
pKd 9.1 (Kd 9x10-10 M) [29]
[3H]5-CT Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Agonist 9.1 pKd 53
pKd 9.1 (Kd 9x10-10 M) [53]
[3H]8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 9.0 pKd 30
pKd 9.0 (Kd 1x10-9 M) [30]
[125I]GTI Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Agonist 8.9 pKd 3-4
pKd 8.9 (Kd 1.3x10-9 M) [3-4]
[3H]alniditan Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.9 – 8.9 pKd 19
pKd 8.9 – 8.9 (Kd 1.4x10-9 – 1.2x10-9 M) [19]
[3H]5-HT Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.2 – 8.6 pKd 19,43,49
pKd 8.2 – 8.6 [19,43,49]
[3H]sumatriptan Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.2 pKd 29
pKd 8.2 (Kd 7x10-9 M) [29]
donitriptan Small molecule or natural product Click here for species-specific activity table Rn Full agonist 9.6 pKi 15
pKi 9.6 [15]
dihydroergotamine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 9.2 – 9.9 pKi 12,19-20
pKi 9.2 – 9.9 [12,19-20]
oxymetazoline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 9.4 pKi 18
pKi 9.4 [18]
donitriptan Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.3 pKi 15
pKi 9.3 [15]
7-methoxy-1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.2 pKi 16
pKi 9.2 [16]
lysergol Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.2 pKi 49
pKi 9.2 [49]
ergotamine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Agonist 9.1 pKi 10
pKi 9.1 (Ki 8x10-10 M) [10]
PNU109291 Small molecule or natural product Gg Agonist 9.1 pKi 8
pKi 9.1 (Ki 9x10-10 M) [8]
alniditan Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.7 – 9.4 pKi 19-20
pKi 8.7 – 9.4 [19-20]
L-694,247 Small molecule or natural product Click here for species-specific activity table Hs Agonist 9.0 pKi 52
pKi 9.0 (Ki 1x10-9 M) [52]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 9.0 pKi 24
pKi 9.0 [24]
ziprasidone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 9.0 pKi 42
pKi 9.0 [42]
5-CT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.6 – 9.2 pKi 12,20,49
pKi 8.6 – 9.2 [12,20,49]
eletriptan Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Full agonist 8.9 pKi 29
pKi 8.9 (Ki 1.26x10-9 M) [29]
zolmitriptan Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Full agonist 8.9 pKi 29
pKi 8.9 [29]
lysergic acid Small molecule or natural product Hs Full agonist 8.8 – 9.0 pKi 20
pKi 8.8 – 9.0 [20]
GR 127935 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 8.6 – 9.1 pKi 9,16,36,43,48
pKi 8.6 – 9.1 [9,16,36,43,48]
naratriptan Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Full agonist 8.4 – 9.0 pKi 7,29,38
pKi 8.4 – 9.0 [7,29,38]
CGS-12066 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.5 – 8.6 pKi 12,49
pKi 8.5 – 8.6 [12,49]
5-hydroxytryptamine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 8.0 – 9.0 pKi 5,12,20,30,43,48-49
pKi 8.0 – 9.0 [5,12,20,30,43,48-49]
asenapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 8.4 pKi 42
pKi 8.4 [42]
frovatriptan Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Agonist 8.4 pKi 54
pKi 8.4 (Ki 4.4x10-9 M) [54]
avitriptan Small molecule or natural product Click here for species-specific activity table Hs Agonist 8.4 pKi 41
pKi 8.4 (Ki 4.37x10-9 M) [41]
sumatriptan Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Full agonist 8.0 – 8.7 pKi 12,20,25,29,49
pKi 8.0 – 8.7 (Ki 1x10-8 – 1.99x10-9 M) [12,20,25,29,49]
xanomeline Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.2 pKi 46
pKi 8.2 [46]
1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.1 – 8.2 pKi 16,49
pKi 8.1 – 8.2 [16,49]
cabergoline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 8.1 pKi 24
pKi 8.1 [24]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.4 – 8.7 pKi 12,20,49
pKi 7.4 – 8.7 [12,20,49]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 8.0 pKi 24
pKi 8.0 [24]
BRL-15572 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Partial agonist 7.9 pKi 36
pKi 7.9 [36]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 7.9 pKi 24
pKi 7.9 [24]
rizatriptan Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Full agonist 7.9 pKi 29
pKi 7.9 [29]
terguride Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 7.8 pKi 24
pKi 7.8 [24]
RU 24969 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.7 pKi 12
pKi 7.7 [12]
SB 216641 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 7.6 pKi 36
pKi 7.6 [36]
aripiprazole Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.2 pKi 44
pKi 7.2 [44]
dimethyltryptamine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.0 – 7.3 pKi 20
pKi 7.0 – 7.3 [20]
TFMPP Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.1 – 7.2 pKi 12,49
pKi 7.1 – 7.2 [12,49]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.9 – 7.3 pKi 7,20,29
pKi 6.9 – 7.3 [7,20,29]
tryptamine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.8 – 7.4 pKi 20,49
pKi 6.8 – 7.4 [20,49]
roxindole Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 7.0 – 7.2 pKi 24,30
pKi 7.0 – 7.2 [24,30]
EMDT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.5 pKi 10
pKi 6.5 [10]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.4 pKi 42
pKi 6.4 [42]
α-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.1 – 6.6 pKi 20
pKi 6.1 – 6.6 [20]
LY344864 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.2 pKi 32
pKi 6.2 [32]
olanzapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.2 pKi 42
pKi 6.2 [42]
2-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.7 – 6.2 pKi 20,49
pKi 5.7 – 6.2 [20,49]
quetiapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 5.7 pKi 42
pKi 5.7 [42]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.1 pKi 27
pKi 5.1 [27]
dipropyl-5-CT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.9 pIC50 49
pIC50 7.9 [49]
almotriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Agonist 7.9 pIC50 2
pIC50 7.9 (IC50 1.3x10-8 M) [2]
Description: Affinity of almotriptan at recombinant h5-HT1D receptors expressed in HeLa cells, determined in a radioligand displacement assay using [125I]GTI as tracer.
CP-122288 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.7 pIC50 7
pIC50 7.7 [7]
View species-specific agonist tables
Agonist Comments
Frovatriptan is selective for 1B and 1D 5-HT receptor subtypes over the 1A subtype [54].
BRL-15572 can be used to distinguish between 5-HT1D and 5-HT1B receptors, being approximately 60-fold selective for the 1D subtype [36].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]GR 125,743 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 8.6 pKd 53
pKd 8.6 (Kd 2.8x10-9 M) [53]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 9.3 pKi 42
pKi 9.3 [42]
SB 714786 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.1 pKi 45
pKi 9.1 (Ki 7.94x10-10 M) [45]
metergoline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 – 9.2 pKi 7,12,20
pKi 8.6 – 9.2 [7,12,20]
SB 649915 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.8 pKi 45
pKi 8.8 [45]
ocaperidone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.7 – 8.8 pKi 20
pKi 8.7 – 8.8 [20]
SB 272183 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.7 pKi 47
pKi 8.7 [47]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.4 – 8.9 pKi 20,49
pKi 8.4 – 8.9 [20,49]
GR 127935 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.3 – 8.6 pKi 20
pKi 8.3 – 8.6 [20]
9-OH-risperidone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.9 pKi 42
pKi 7.9 [42]
risperidone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.8 – 8.0 pKi 20,42
pKi 7.8 – 8.0 [20,42]
bufotenine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.7 – 8.0 pKi 20
pKi 7.7 – 8.0 [20]
rauwolscine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.8 pKi 49
pKi 7.8 [49]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 7.3 – 8.2 pKi 7,12,20,48
pKi 7.3 – 8.2 [7,12,20,48]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.6 pKi 20
pKi 7.6 [20]
(+)-WAY 100135 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.6 pKi 5
pKi 7.6 [5]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.4 – 7.5 pKi 7,20
pKi 7.4 – 7.5 [7,20]
yohimbine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.2 – 7.7 pKi 12,20,25,49
pKi 7.2 – 7.7 [12,20,25,49]
sertindole Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.2 pKi 42
pKi 7.2 [42]
cyanopindolol Small molecule or natural product Hs Antagonist 7.1 pKi 12
pKi 7.1 [12]
S33084 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.9 pKi 23
pKi 6.9 [23]
pipamperone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 pKi 42
pKi 6.8 [42]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.7 pKi 12
pKi 6.7 [12]
haloperidol Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.6 pKi 42
pKi 6.6 [42]
SB 224289 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 pKi 9,43
pKi 6.3 [9,43]
fluspirilene Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.0 pKi 42
pKi 6.0 [42]
SB 277011-A Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.8 pKi 37
pKi 5.8 [37]
spiperone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.5 – 6.0 pKi 12,49
pKi 5.5 – 6.0 [12,49]
MPDT Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.2 pKi 10
pKi 5.2 [10]
L-772,405 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.0 pIC50 40
pIC50 9.0 [40]
vortioxetine Small molecule or natural product Approved drug Immunopharmacology Ligand Rn Antagonist 5.4 pIC50 13
pIC50 5.4 (IC50 4x10-6 M) [13]
View species-specific antagonist tables
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
5-HT-moduline Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Negative 12.0 pIC50 39
pIC50 12.0 [39]
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  12,21
Tissue Distribution Click here for help
Trigeminal ganglion.
Species:  Human
Technique:  immunocytochemistry.
References:  14
Spinal cord: dorsal horn > ventral horn.
Species:  Human
Technique:  Radioligand binding.
References:  17
Poorly expressed in coronary arteries, atrium, ventricle and epicardium.
Species:  Human
Technique:  RT-PCR.
References:  31
Benign and malignant prostate tissue.
Species:  Human
Technique:  Western blotting.
References:  6
Globus pallidus > frontal cortex > putamen.
Species:  Human
Technique:  Radioligand binding.
References:  26
Trigeminal ganglion.
Species:  Rat
Technique:  Immunohistochemistry.
References:  22
Dorsal root ganglion and trigeminal ganglion.
Species:  Rat
Technique:  immunocytochemistry.
References:  35
Lumbar dorsal root ganglia, superior cervical ganglia, lumbar sympathetic ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  33
Expression Datasets Click here for help

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays Click here for help
Measurement of cAMP levels in mouse adrenal Y-1 cells transfected with the 5-HT1D receptor.
Species:  Human
Tissue:  Y-1 cells.
Response measured:  Inhibition of cAMP accumulation.
References:  49
Physiological Functions Click here for help
Growth hormone release.
Species:  Human
Tissue:  In vivo.
References:  28,51
Inhibition of 5-HT release.
Species:  Rat
Tissue:  in vivo and mesencephalic raphe slices.
References:  34
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Htr1dtm1Lex Htr1dtm1Lex/Htr1dtm1Lex
involves: 129S5/SvEvBrd * C57BL/6J
MGI:96276  MP:0002169 no abnormal phenotype detected
Biologically Significant Variants Click here for help
Type:  Single nucleotide polymorphisms
Species:  Human
Description:  Three polymorphisms, 1123 T -> G, 628 T-> C and 2190 A -> G have a possible association with anorexia nervosa.
References:  1

References

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1. Bergen AW, van den Bree MB, Yeager M, Welch R, Ganjei JK, Haque K, Bacanu S, Berrettini WH, Grice DE, Goldman D et al.. (2003) Candidate genes for anorexia nervosa in the 1p33-36 linkage region: serotonin 1D and delta opioid receptor loci exhibit significant association to anorexia nervosa. Mol. Psychiatry, 8 (4): 397-406. [PMID:12740597]

2. Bou J, Domènech T, Puig J, Heredia A, Gras J, Fernández-Forner D, Beleta J, Palacios JM. (2000) Pharmacological characterization of almotriptan: an indolic 5-HT receptor agonist for the treatment of migraine. Eur. J. Pharmacol., 410 (1): 33-41. [PMID:11134654]

3. Boulenguez P, Segu L, Chauveau J, Morel A, Lanoir J, Delaage M. (1992) Biochemical and pharmacological characterization of serotonin-O-carboxymethylglycyl[125I]iodotyrosinamide, a new radioiodinated probe for 5-HT1B and 5-HT1D binding sites. J. Neurochem., 58 (3): 951-9. [PMID:1738002]

4. Bruinvels AT, Palacios JM, Hoyer D. (1993) Autoradiographic characterisation and localisation of 5-HT1D compared to 5-HT1B binding sites in rat brain. Naunyn Schmiedebergs Arch. Pharmacol., 347 (6): 569-82. [PMID:8361548]

5. Davidson C, Ho M, Price GW, Jones BJ, Stamford JA. (1997) (+)-WAY 100135, a partial agonist, at native and recombinant 5-HT1B/1D receptors. Br. J. Pharmacol., 121 (4): 737-42. [PMID:9208142]

6. Dizeyi N, Bjartell A, Nilsson E, Hansson J, Gadaleanu V, Cross N, Abrahamsson PA. (2004) Expression of serotonin receptors and role of serotonin in human prostate cancer tissue and cell lines. Prostate, 59 (3): 328-36. [PMID:15042609]

7. Doménech T, Beleta J, Palacios JM. (1997) Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist. Naunyn Schmiedebergs Arch. Pharmacol., 356 (3): 328-34. [PMID:9303569]

8. Ennis MD, Ghazal NB, Hoffman RL, Smith MW, Schlachter SK, Lawson CF, Im WB, Pregenzer JF, Svensson KA, Lewis RA et al.. (1998) Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects. J. Med. Chem., 41 (13): 2180-3. [PMID:9632349]

9. Gaster LM, Blaney FE, Davies S, Duckworth DM, Ham P, Jenkins S, Jennings AJ, Joiner GF, King FD, Mulholland KR et al.. (1998) The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo. J. Med. Chem., 41 (8): 1218-35. [PMID:9548813]

10. Glennon RA, Lee M, Rangisetty JB, Dukat M, Roth BL, Savage JE, McBride A, Rauser L, Hufeisen S, Lee DK. (2000) 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J. Med. Chem., 43 (5): 1011-8. [PMID:10715164]

11. Hamblin MW, McGuffin RW, Metcalf MA, Dorsa DM, Merchant KM. (1992) Distinct 5-HT1B and 5-HT1D serotonin receptors in rat: structural and pharmacological comparison of the two cloned receptors. Mol. Cell. Neurosci., 3: 578-587.

12. Hamblin MW, Metcalf MA. (1991) Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor. Mol. Pharmacol., 40 (2): 143-8. [PMID:1652050]

13. Heinrich T, Böttcher H, Gericke R, Bartoszyk GD, Anzali S, Seyfried CA, Greiner HE, Van Amsterdam C. (2004) Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors. J. Med. Chem., 47 (19): 4684-92. [PMID:15341484]

14. Hou M, Kanje M, Longmore J, Tajti J, Uddman R, Edvinsson L. (2001) 5-HT(1B) and 5-HT(1D) receptors in the human trigeminal ganglion: co-localization with calcitonin gene-related peptide, substance P and nitric oxide synthase. Brain Res., 909 (1-2): 112-20. [PMID:11478927]

15. John GW, Pauwels PJ, Perez M, Halazy S, Le Grand B, Verscheure Y, Valentin JP, Palmier C, Wurch T, Chopin P et al.. (1999) F 11356, a novel 5-hydroxytryptamine (5-HT) derivative with potent, selective, and unique high intrinsic activity at 5-HT1B/1D receptors in models relevant to migraine. J. Pharmacol. Exp. Ther., 290 (1): 83-95. [PMID:10381763]

16. Jorand-Lebrun C, Pauwels PJ, Palmier C, Moret C, Chopin P, Perez M, Marien M, Halazy S. (1997) 5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine. J. Med. Chem., 40 (24): 3974-8. [PMID:9397179]

17. Laporte AM, Doyen C, Nevo IT, Chauveau J, Hauw JJ, Hamon M. (1996) Autoradiographic mapping of serotonin 5-HT1A, 5-HT1D, 5-HT2A and 5-HT3 receptors in the aged human spinal cord. J. Chem. Neuroanat., 11 (1): 67-75. [PMID:8841890]

18. Law H, Dukat M, Teitler M, Lee DK, Mazzocco L, Kamboj R, Rampersad V, Prisinzano T, Glennon RA. (1998) Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation. J. Med. Chem., 41 (13): 2243-51. [PMID:9632357]

19. Lesage AS, Wouters R, Van Gompel P, Heylen L, Vanhoenacker P, Haegeman G, Luyten WH, Leysen JE. (1998) Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. Br. J. Pharmacol., 123 (8): 1655-65. [PMID:9605573]

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